Product News | ACS Fall 2023 Big Pharma R&D Update (1/3)

Sep.08.2023

The American Chemical Society's (ACS) 2023 Annual Meeting was held in San Francisco, USA, from 13 to 17 August, with the theme of Harnessing the Power of Data.As a major international meeting of the chemical industry, ACS attracts the attention of chemists from all over the world, and during the meeting, pharmaceutical companies will also announce their latest research results.

KIN-3248

(Kinnate Biopharma)

FGFRs (Fibroblast Growth Factor Binding Receptors) play an important role in both pro- and non-promotional biological processes, such as embryogenesis, growth and development, etc. Overexpression of FGFRs, mutations and other abnormalities can lead to the activation of their signalling pathways, which can lead to uncontrolled pro-promotional effects and tumour triggering.

Currently, there are three commonly used FGFR-targeted drugs in the clinic: FGFR2-targeted inhibitor Pemigatinib, FGFR2/3-targeted inhibitor Erdafitinib and pan-FGFR inhibitor Futibatinib.

With the proliferation of FGFR-targeted drugs, the problem of drug-resistant mutations in FGFR proteins has become more pronounced, and in response, Kinnate Biopharma has designed KIN-3248, a pan-FGFR inhibitor, specifically to target drug-resistant mutations such as FGFR2V565F, FGFR3V555M, and FGFR2N550K. Currently, KIN-3248 is in Phase 1 at its highest clinical development status, with indications encompassing both FGFR2-mutant and FGFR3-mutant tumours.

NX-5948

(Nurix Theraputic)

BTK (Bruton's tyrosine kinase), expressed in a wide range of haematological cells, plays an important role in physiological processes such as differentiation, maturation and signalling of B lymphocytes, and has a high correlation with B-cell tumourigenesis.

Nurix Theraputic has designed a PROTAC drug: NX-5948, which is capable of targeting and degrading BTK. The above drug has shown promising therapeutic efficacy in common diffuse large B-cell lymphoma as well as Ibrutinib-resistant diffuse large B-cell lymphoma mouse models. In addition, NX-5948 crosses the blood-brain barrier and also exhibits good tumour inhibitory activity in a mouse model of cerebral lymphoma. NX-5948 is currently in Phase 1 clinical development for the treatment of BTK-related cancers such as B-cell chronic lymphocytic leukaemia.

KT-474

(Kymera Therapeutics)

IRAK4 is a key protein involved in inflammation, mediated by the Toll-like receptor (TLR) and IL-1 receptor (IL-1R), and aberrant activation of these pathways is the underlying cause of a wide range of immune-inflammatory diseases.IRAK4 degraders may play a role in the treatment of autoimmune diseases.

The oral IRAK4 PROTAC: KT-474, designed by Kymera Theraputic, is intended for the treatment of inflammatory and autoimmune diseases, including atopic dermatitis, hidradenitis suppurativa and rheumatoid arthritis. Interim results from previously announced Phase 1 clinical trials showed that adequate doses of KT-474 reduced IRAK levels in peripheral blood mononuclear cells by 93-96%. The current highest development status of KT-474 is clinical phase 1, primarily for the treatment of autoimmune diseases such as atopic dermatitis.

STC-15

(STROM Therapeutics)

STROM Therapeutics is the first company to focus on RNA modifying enzymes as drug targets.METTL3 is an RNA methyltransferase responsible for m6A (N6-methyladenosine) modification on RNA molecules.Elevated expression of METTL3 leads to aberrant m6A modification, which affects the transcriptional and translational processes of specific genes and ultimately triggers leukaemia development and progression. ultimately triggers the development and progression of leukaemia.STC-15 is a newest METTL3 inhibitor with a current clinical development status of phase 1, mostly used for the treatment of haematological tumours.

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NX-5948

(Nurix Theraputic)